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A major hurdle in pharmaceutical formulation is water insolubility of most of the drugs affecting stability and bioavailability of the drug, if the drug is also insoluble in organic medium, it is difficult to deliver the drug in a sufficiently bioavailable form and hence it is a great challenge to formulation researchers to overcome such difficulty. Although some approaches are available for enhancing the dissolution of poorly soluble drugs but has certain draw backs like low drug loading and large doses. However, a new solution to poorly water soluble drug candidates is now available i.e. nanonisation and it leads to much more soluble, more biologically available and safer dosage form of poorly soluble and poorly bioavailable drugs. In the present work, a nanocrystal of lovastatin was formulated by using simple precipitation method without using stabilizer or surfactant and it was found that formulation at 3 mM concentration of drug with the acetone and methanol as a solvent and at proper dilution (50 times) of drug solution with water, nanocrystals with less particle size is possible with slight change in crystallinity. It has also shown that, the drug has enhanced saturation solubility, increased dissolution rate and more bioavailable in biological fluid when drug formulated by using acetone and methanol as a solvent. Whereas drug formulation with acetonitrile has large particle size, less saturation solubility and low rate of dissolution.

Objective: To prepare and characterize Albumin microspheres of hydralazine hydrochloride for the treatment of hypertension. Methods: Albumin microspheres of antihypertensive drug hydralazine hydrochloride were prepared by emulsion cross-linking method by using glutaraldehyde as cross-linking agent. Drug and polymer compatibility was determined by Fourier-Transform Infrared spectroscopy. To determine the effect of polymer concentration and amount of glutaraldehyde, formulations were characterized for their entrapment efficiency, particle size, surface morphology and release behavior. In vivo study was carried out on hypertensive wistar rats. Key findings: Maximum percentage entrapment efficiency (%EE) was found to be 68.20±1.03 %. Laser particle size analyzer confirmed mean particle size in the range of 31.7 to 39.6μm. In vitro drug release studies showed a biphasic release pattern for all formulations with an initial burst effect followed by slow release for almost 24 hrs. Conclusion: In vivo study to determine antihypertensive effect of selected formulation strongly correlates with in vitro drug release behavior. The release behavior was significantly regulated by polymer concentration and volume of glutaraldehyde. The study revealed that hydralazine hydrochloride loaded albumin microspheres exhibited prolonged reduction of systolic and diastolic arterial pressure compared to hydralazine hydrochloride solution.

The present study is aimed at the overall improvement in the efficacy, reduced toxicity and enhancement of therapeutic index of cisplatin. Solid lipid nanoparticulate delivery system of cisplatin has been developed by microemulsification method by using stearic acid, soy lecithin 95% and sodium glycolate. The formulations were then characterized with respect to size and its surface morphology, zeta potential, entrapment efficiency, in vitro drug release profile, in vivo drug targeting studies and its stability under specific conditions. The formulated solid lipid nanoparticles were oval with a diameter ranging from 250 nm to 500 nm. The lowest entrapment efficiency was found to be 47.59% and highest was found to be 74.53%. The zeta potential was in the range of -9.8 to -11.2 mv. In vitro release study was analyzed using various mathematical models. Highest cumulative percent drug release was observed with F-1 (97.22 %) and lowest with F-4 (78.43%) in 16 h. The in vivo result of formulated solid lipid nanoparticles of cisplatin reveals that the drug is preferentially targeting to liver followed by brain and lungs.